Topic
Tolibut
About: Tolibut is a research topic. Over the lifetime, 3 publications have been published within this topic receiving 2 citations. The topic is also known as: 4-amino-3-(4-methylphenyl)butanoic acid.
Papers
TL;DR: GABA analogs containing phenyl (phenibut) or para-chlorophenyl (baclofen) substituents demonstrated nootropic activity in a dose of 20 mg/kg and demonstrated neuroprotective properties on the maximum electroshock model: they shortened the duration of coma and shortened the period of spontaneous motor activity recovery.
Abstract: GABA analogs containing phenyl (phenibut) or para-chlorophenyl (baclofen) substituents demonstrated nootropic activity in a dose of 20 mg/kg: they improved passive avoidance conditioning, decelerated its natural extinction, and exerted antiamnestic effect on the models of amnesia provoked by scopolamine or electroshock. Tolyl-containing GABA analog (tolibut, 20 mg/kg) exhibited antiamnestic activity only on the model of electroshock-induced amnesia. Baclofen and, to a lesser extent, tolibut alleviated seizures provoked by electroshock, i.e. both agents exerted anticonvulsant effect. All examined GABA aryl derivatives demonstrated neuroprotective properties on the maximum electroshock model: they shortened the duration of coma and shortened the period of spontaneous motor activity recovery. In addition, these agents decreased the severity of passive avoidance amnesia and behavioral deficit in the open field test in rats exposed to electroshock. The greatest neuroprotective properties were exhibited by phenyl-containing GABA analog phenibut.
7 citations
Journal Article•
TL;DR: In this article, the analgetic activity of baclofen and tolibut (2.5-10.0 mg/kg) was studied in experiments on albino mice and rats and showed a dose-dependent inhibition of perceptive, emotional and autonomic manifestations of nociceptive reactions at the tail's thermal and electrical stimulation.
Abstract: Spectrum of the analgetic activity of GABA derivatives baclofen (2.5-10.0 mg/kg) and tolibut (12.5-100.0 mg/kg) was studied in experiments on albino mice and rats. Baclofen and especially tolibut showed a dose-dependent inhibition of perceptive, emotional and autonomic manifestations of nociceptive reactions at the tail's thermal and electrical stimulation and enhancement of the analgetic effect of promedol. The regressive analysis made it possible to show dependence of the analgetic effect on the level of pain sensitivity and emotional reactivity of the animals. Tolibut deepens and prolongs sombrevin anesthesia, baclofen fails to alter it.
1 citations
TL;DR: In this paper, a 3-substituted 4-(1H-tetrazol-1-yl)butanoic acids, analogs of the neurotropic drugs phenibut, tolibut, and baclofen, were synthesized by a three-component reaction of the R-isomers of corresponding amino acids, triethyl orthoformate, and sodium azide.
Abstract: Nonracemic 3-substituted 4-(1H-tetrazol-1-yl)butanoic acids, analogs of the neurotropic drugs phenibut, tolibut, and baclofen, were synthesized by a three-component reaction of the R-isomers of the corresponding amino acids, triethyl orthoformate, and sodium azide. The key stage of the synthesis is the asymmetric addition of diethyl malonate to nitroalkenes, catalyzed by a Ni(II) complex of (S,S)-N,N′-dibenzylcyclohexane-1,2-diamine.
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2018 | 1 |
| 2016 | 1 |
| 1987 | 1 |